Novel boron-based compounds (BBCs) were synthesized and evaluated as potential candidates for the development of novel drugs against Alzheimer's disease (AD). The neuroprotective profile of novel BBCs was evaluated using Aβ1-42-treated-SH-SY5Y cells while their antioxidant activity was evaluated by total antioxidant capacity (TAC) and total oxidative status (TOS) assays. Results showed that BLA (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by Aβ1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in cell viability by 25–33% (MTT assay) and by 63–71% (LDH assay) in a concentration range of 25–100 μM. Antioxidant assays demonstrated a good capability of BLA to counteract the oxidative status. Moreover, BLA possessed a significant ability to inhibit acetylcholinesterase (AChE) (22.96% at 50 μM), an enzyme whose enzymatic activity is increased in AD patients. In the present work, absorption and distribution properties of boron-based hybrids were predicted using Pre-ADMET software. In vitro preliminary results suggested that boron-based hybrids could be new structural scaffolds for the development of novel drugs for the management of AD.

中文翻译：

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硼基杂化物作为新型支架用于开发具有神经保护特性的药物

合成了新型硼基化合物（BBC），并将其作为开发抗阿尔茨海默病（AD）新药的潜在候选药物进行了评估。使用 Aβ1-42 处理的 SH-SY5Y 细胞评估新型 BBC 的神经保护作用，同时通过总抗氧化能力 (TAC) 和总氧化状态 (TOS) 测定评估其抗氧化活性。结果表明，BLA（一种含有抗氧化剂部分的新型硼基杂化物）可抑制分化的 SH-SY5Y 细胞中 Aβ1-42 暴露诱导的细胞死亡，导致细胞活力增加 25-33%（MTT 测定）在 25–100 μM 浓度范围内，提高 63–71%（LDH 测定）。抗氧化测定表明BLA具有良好的抵抗氧化状态的能力。此外，BLA具有显着的抑制乙酰胆碱酯酶 (AChE) 的能力（50 μM 时为 22.96%），这种酶的酶活性在 AD 患者中增加。在目前的工作中，使用 Pre-ADMET 软件预测了硼基杂化物的吸收和分布特性。体外初步结果表明，硼基杂化物可以成为开发治疗 AD 的新药物的新结构支架。